Enhanced tumor-targeted delivery of anticancer drugs by folic acid-conjugated pH-sensitive polymeric micelles

作     者：Chuhang Zhou Xinping Hu Qi Liu Leqi Wang Yuanhang Zhou Yao Jin Yan Liu 周楚杭;胡新平;刘琦;王乐淇;周远航;靳尧;刘艳

作者机构：Beijing Key Laboratory of Molecular Pharmaceutics and New Dmg Delivery SystemsSchool of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China 

基　　金：National Natural Science Foundation of China(Grant No.81673366) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2020年第29卷第9期

页      码：626-636页

摘      要：In order to enhance the targeted delivery of anticancer drugs by polymeric micelles, folic acid(FA), the ligand of folate receptor(FR) over-expressed in the most cancer cells, modified p H-sensitive polymeric micelles were designed and fabricated to encapsulate doxorubicin(DOX) by combination of p H-sensitive amphiphilic polymer poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) with FA-conjugated poly(2-ethyl-2-oxazoline)-poly(D,L-lactide). The prepared micelles were characterized to have about 36 nm in diameter with narrow distribution, well-defined spherical shape observed under TEM and p H-responsive drug release behavior. Moreover, the tumor targeting ability of the FA-modified p H-sensitive polymeric micelles was demonstrated by the cellular uptake, in vitro cytotoxicity to FR-positive KB cells and in vivo real time near-infrared fluorescence imaging in KB tumor-bearing nude mice. The efficient drug delivery by the micelles was ascribed to the synergistic effects of FR-mediated targeting and p H-triggered drug release. In conclusion, the designed FR-targeted p H-sensitive polymeric micelles might be of great potential in tumor targeted delivery of water-insoluble anticancer drugs.

主 题 词：pH-sensitive polymeric micelles Folate receptor-targeted Tumor-targeted delivery Cell uptake Doxorubicin 

学科分类：100702[100702] 1007[医学-药学类] 1006[医学-中西医结合类] 100602[100602] 10[医学] 

核心收录：

D　O　I：10.5246/jcps.2020.09.058

馆 藏 号：203979150...